Drug Groups

illicit; experimental

Description

A narcotic analgesic that may be habit-forming. It is a controlled substance (opium derivative) listed in the U.S. Code of Federal Regulations, Title 21 Parts 329.1, 1308.11 (1987). Sale is forbidden in the United States by Federal statute. (Merck Index, 11th ed) Internationally, heroin is controlled under Schedules I and IV of the Single Convention on Narcotic Drugs. It is illegal to manufacture, possess, or sell heroin in the United States and the UK. However, under the name diamorphine, heroin is a legal prescription drug in the United Kingdom.

Indication

Used in the treatment of acute pain, myocardial infarction, acute pulmonary oedema, and chronic pain.

Pharmacology

The onset of heroin's effects is dependent on the method of administration. Taken orally, heroin is totally metabolized in vivo into morphine before crossing the blood-brain barrier; so the effects are the same as oral morphine. Take by injection, heroin crosses into the brain. Once in the brain, heroin is rapidly metabolized into morphine by removal of the acetyl groups, therefore, it is known as a prodrug. It is the morphine molecule that then binds with opioid receptors and produces the subjective effects of the heroin high.

Affected Organisms

Biotransformation

Hepatic.

Absorption

Bioavailability is less than 35%.

Half Life

2-3 hours

Protein Binding

0% (morphine metabolite 35%)

Elimination

90% renal as glucuronides, rest biliary

References

External Links